Selection of DNA-Encoded Libraries to Protein Targets within and on Living Cells
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, cilt.141, sa.43, ss.17057-17061, 2019 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 141 Sayı: 43
- Basım Tarihi: 2019
- Doi Numarası: 10.1021/jacs.9b08085
- Dergi Adı: JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.17057-17061
- Orta Doğu Teknik Üniversitesi Adresli: Hayır
Özet
We report the selection of DNA-encoded small molecule libraries against protein targets within the cytosol and on the surface of live cells. The approach relies on generation of a covalent linkage of the DNA to protein targets by affinity labeling. This cross-linking event enables subsequent copurification by a tag on the recombinant protein. To access targets within cells, a cyclic cell-penetrating peptide is appended to DNA-encoded libraries for delivery across the cell membrane. As this approach assesses binding of DELs to targets in live cells, it provides a strategy for selection of DELs against challenging targets that cannot be expressed and purified as active.